泛昔洛韦片的人体生物等效性研究

Bioequivalence of Famciclovir Tablets in Chinese healthy volunteers

目的研究泛昔洛韦片的人体相对生物利用度和生物等效性。方法健康志愿者20名,随机双交叉单剂量口服泛昔洛韦片(试验和参比制剂),剂量分别为0.5 g,剂间间隔为1周。分别于服药后12 h内多点抽取静脉血;用高效液相色谱(HPLC)法测定血浆中喷昔洛韦的浓度。用DAS药代动力学程序计算相对生物利用度并评价两种制剂生物等效性。AUC_(0-12)),AUC_((0-∞)和和Cmax经方差分析和双单侧t检验,Tmax进行秩和检验。结果单剂量口服泛昔洛韦试验和参比制剂后,血浆喷昔洛韦的Cmax分别为(2.92±0.76)mg·L^(-1)和(2.98±1.00)mg·L^(-1);Tmax分别为(1.04±0.46)h和(1.17±0.61)h;AUC_((0-12)分别为(8.51±2.46)mg·h·L^(-1)和(8.73±2.86)mg·h·L^(-1);AUC_((0-∞)分别为(8.87±2.57)mg·h·L^(-1)和(9.10±2.99)mg·h·L^(-1)。AUC_((0-12))AUC_((0-∞))和Cmax的90%可信区间分别为83.9%～99.6%、83.5%～99.2%和92.4%～108.1%。结论试验制剂的相对生物利用度为(97.53±18.49)%;两制剂具有生物学等效性。

OBJECTIVE To study the relative bioavailability and bioequivalence of Famciclovir Tablets in healthy volunteers.METHODS A single oral dose （0.5 g of tested and reference formulation） were given to 20 healthy volunteers in a randomised crossover study. The concentrations of penciclovir in plasma were determined by HPLC. The pharmacokinetics parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. RESULTS After a single dose, the pharmacokinetics parameters for penciclovir were as follows： Cmax were （2.92 ± 0.76） mg·L^-1 and （2.98± 1.00）mg·L^-1; Tmax were （ 1.04 ± 0.46） h and （1.17 ± 0.61） h; AUC（0-12） were （8.51 ± 2.46） mg/（h· L） and （8.73 ± 2.86） mg/（h·L）; AUC（0-∞） were （8.87 ±2.57） mg/（h·L） and （9.10 ± 2.99） mg/（h·L） for tested and reference formulation respectively. The 90 % confidential interval of AUC（0-12）,AUC（0-∞） and Cmax of tested formulation were 83.9 % 99.6%, 83.5% - 99.2% and 92.4% -108.1% respectively.COCLUSION The relative bioavailability was （97.53 ± 18.49） % ; The results of the statistic analysis showed that the two formulations were bioequivalence.